About 30 results found for searched term "MAPK-IN-2" (0.108 seconds)
Cat.No. | Name | Target |
---|---|---|
M42115 | MAPK-IN-2 | EGFR/HER2 |
MAPK-IN-2 is a potent MAPK inhibitor with antineoplastic activity. | ||
M1977 | U0126-EtOH | MEK |
U0126 | ||
U0126-EtOH is a potent and highly selective non-competitive inhibitor of MAPK/ERK kinase with IC50 of 72 nM for MEK1 and 58 nM for MEK2. | ||
M2090 | MLN2480 | Raf |
BIIB-024; Tovorafenib | ||
MLN2480 is an orally active, CNS-permeable, highly selective inhibitor of type II RAF kinase that inhibits both monomeric (class I mutant) and dimeric forms of RAF and does not cause aberrant activation of the MAPK pathway caused by type I RAF inhibitors. In addition, MLN2480 inhibits the growth of tumors harboring BRAF fusions or BRAF V600 mutations and can be used in studies related to gliomas. | ||
M2198 | Curcumin | Histone Acetyltransferase |
Indian Saffron; Turmeric yellow; Natural Yellow 3; Diferuloylmethane | ||
Curcumin (Diferuloyl), a natural phenolic compound, is a p300/CREB binding protein specific inhibitor that inhibits histone/non-histone acetylation and histone acetyltransferase-dependent chromatin transcription. Curcumin inhibited NF-κ B and MAPKs, and had anti-inflammatory, antioxidant, anti-proliferation and anti-angiogenesis effects. Curcumin induces Nrf2 protein stabilization through Keap1 cysteine modification. | ||
M3048 | TAK-715 | p38 MAPK |
TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. | ||
M5873 | Pexmetinib (ARRY-614) | p38 MAPK |
ARRY-614 | ||
Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1. | ||
M6146 | TA-02 | p38 MAPK |
TA 02; TA02 | ||
TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2. | ||
M6661 | Deguelin | Akt |
(-)-Deguelin; (-)-cis-Deguelin | ||
Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB. | ||
M7582 | SB 239063 | p38 MAPK |
SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580. | ||
M7792 | EF-24 | ERK |
EF24 | ||
EF-24 is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. | ||
M9692 | IAXO-102 | TLR |
Iaxo-102 is an antagonist of TLR4 and inhibits the TLR4 signaling pathway. Iaxo-102 inhibits phosphorylation of MAPK and P65 NF-KB and expression of TLR4 and TLR4-dependent inflammatory proteins. Iaxo-102 inhibits the development of experimental abdominal aortic aneurysms. | ||
M14174 | BMS-582949 hydrochloride | p38 MAPK |
BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease. | ||
M14176 | MAPK13-IN-1 | p38 MAPK |
MPAK13-IN-1 is a MAPK13 (p38δ) inhibitor, with an IC50 of 620 nM. | ||
M14177 | p38-α MAPK-IN-1 | p38 MAPK |
p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay. | ||
M20012 | CC-99677 | Others |
CC-99677 is an oral, covalent MAPK–activated protein kinase-2 (MK2) inhibitor being developed for autoimmune diseases. | ||
M21938 | BCI-215 | Phosphatase |
BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells. | ||
M28107 | PF-3644022 | MAPKAPK2/MAP3K/MAP4K |
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect. | ||
M28723 | MW-150 | p38 MAPK |
MW01-18-150SRM | ||
MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia. | ||
M28785 | MW-150 dihydrochloride dihydrate | p38 MAPK |
MW01-18-150SRM dihydrochloride dihydrate | ||
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia. | ||
M28792 | SD-169 | p38 MAPK |
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation. | ||
M28863 | PD-089828 | FGFR |
PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity. | ||
M29024 | MW-150 hydrochloride | p38 MAPK |
MW01-18-150SRM hydrochloride | ||
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia. | ||
M29320 | SHP2-IN-6 | Phosphatase |
JAB-3068 | ||
SHP2-IN-6 is a potent SHP2 inhibitor that interferes with the MAPK signaling pathway and inhibits the proliferation of SHP2-expressing tumor cells with an IC50 value of 25.8 nM. | ||
M29321 | SHP2-IN-6 hydrochloride | Phosphatase |
JAB-3068 hydrochloride | ||
SHP2-IN-6 hydrochloride is a potent SHP2 inhibitor that interferes with the MAPK signaling pathway and inhibits the proliferation of SHP2-expressing tumor cells with an IC50 value of 25.8 nM. | ||
M29615 | SR-318 | p38 MAPK |
SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity. | ||
M30587 | Emprumapimod | p38 MAPK |
PF-07265803 | ||
Emprumapimod (PF-07265803) is a potent, orally active and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain. | ||
M30703 | 12-Oxo phytodienoic acid | NF-κB |
12-OPDA | ||
12-Oxo phytodienoic acid (12-OPDA, 12-oxo phytodienoic acid) is a plant lipid-derived compound with anti-inflammatory activity that inhibits neuroinflammation by inhibiting Nf-κB and p38 MAPK signaling in cells activated by lipopolysaccharide (LPS).12-Oxo phytodienoic acid can be used in the study of neurodegenerative diseases. | ||
M30721 | Ralimetinib | p38 MAPK |
LY2228820 | ||
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc. | ||
M39013 | Broussonin E | ERK |
Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis. | ||
M45287 | CK2/ERK8-IN-1 | Casein Kinase |
CK2/ERK8-IN-1 is a dual inhibitor of casein kinase 2 (CK2) (Ki 0.25 µM) and ERK8 (MAPK15, ERK7), both with IC50s of 0.50 µM. In addition, CK2/ERK8-IN-1 binds to PIM1, HIPK2, and DYRK1A with Ki values of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. 15.25 µM and 11.9 µM, respectively, and also has pro-apoptotic activity. |
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